Deep visceral pain is frequent and presents major challenges in pain management, since its pathophysiology is still poorly understood. One way to optimize treatment of visceral pain is to improve knowledge of the mech...Deep visceral pain is frequent and presents major challenges in pain management, since its pathophysiology is still poorly understood. One way to optimize treatment of visceral pain is to improve knowledge of the mechanisms behind the pain and the mode of action of analgesic substances. This can be achieved through stand-ardized experimental human pain models. Experimental pain models in healthy volunteers are advantageous for evaluation of analgesic action, as this is often diff icult to assess in the clinic because of confounding factors such as sedation, nausea and general malaise. These pain models facilitate minimizing the gap between knowledge gained in animal and human clinical studies. Combining experimental pain studies and pharmacokinetic stud- ies can improve understanding of the pharmacokinetic-pharmacodynamic relationship of analgesics and, thus, provide valuable insight into optimal clinical treatment of visceral pain. To improve treatment of visceral pain, it is important to study the underlying mechanisms of pain and the action of analgesics used for its treatment. An experimental pain model activates different modalities and can be used to investigate the mechanism of action of different analgesics in detail. In combination with pharmacokinetic studies and objective assessment such as electroencephalography, new information re-garding a given drug substance and its effects can be obtained. Results from experimental human visceral pain research can bridge the gap in knowledge between animal studies and clinical condition in patients suffering from visceral pain, and thus constitute the missing link in translational pain research.展开更多
AIM: To investigate the antitumor and synergistic effect of Chinese medicine “Bushen huayu jiedu recipe” (recipe for invigorating the kidney, removing blood stasis and toxic substances) and chemotherapy on mice h...AIM: To investigate the antitumor and synergistic effect of Chinese medicine “Bushen huayu jiedu recipe” (recipe for invigorating the kidney, removing blood stasis and toxic substances) and chemotherapy on mice hepatocarcinoma. METHODS: Bushen huayu jiedu recipe (BSHYJDR) consisting of Chinese Cassia Bark, Psoralea, Zedoary, Rhubarb, etc. is equal to 1.5 g/mL liquid of originated herbs after being decoded, filtered, and concentrated. Kunming mice, weighing 18-22 g, were injected with 0.2 mL ascitic hepatocarcinoma H22 containing 1 × 10^7 cells/mL into armpit of the right forelimb of mice. After 24 h, the mice were weighed and randomly divided into tumor-bearing model control group, cisplatin (DDP) group, BSHYJDR high dosage group, low dosage BSHYJDR group, DDP combined with high and low dosage BSHYJDR group, 10 mice in each group. DDP group received injection intraperitoneally (ip) at the dosage of 1 mg/kg (equal to 1/10 LD50), once a day for 4 d. High and low dosage BSHYJDR groups received intragastric BSHYJDR at the dosages of 26.6 and 13.3 g/kg (20 and 10 times each of clinical adult dosage) respectively, while tumor-bearing model group received the equal volume of distilled water once a day for 10 d. On the 11^th d, the mice were weighed and killed, then the tumor was dissected and weighed, the repression rate (RR) was calculated according to the mean weight of tumor (MWT). RESULTS: Compared to the model group (MWT: 1.30±0.73), DDP group (MWT: 0.41±0.09, RR: 68.46%) had a significant difference in the inhibition of hepatocarcinoma H22 (P〈0.01). High dosage BSHYJDR group (MWT: 0.69±0.29, RR: 46.92%) also had a significant difference in inhibition (P〈0.05), while no difference was found in low dosage BSHYJDR group (MVVT: 0.85±0.34, RR: 34.62%) (P〉0.05). When DDP was combined with high dosage BSHYJDR (MWT: 0.29±0.17, RR: 77.69%) and low dosage BSHYJDR (MWT: 0.38±0.21, RR: 70.77%) respectively, we could see improvement of the inhibition effect of DDP on transplanted hepatocarcinoma H22. DDP combined with high dosage BSHYJDR had a significant difference (P〈0.001) compared to DDP, while DDP combined with low dosage BSHYJDR only had a little improvement that is not remarkable. CONCLUSION: Chinese medicine BSHYJDR in combination with chemotherapy can inhibit transplanted hepatocarcinorna in mice.展开更多
A novel oleanane-type triterpenic acid was isolated from the leaves of Gymnema sylvestre(Asclepiadaceae). The structure was characterized as 3β, 16β, 22β, 28-tetrahydroxy- olean-12-en-30-oic acid on the basis of sp...A novel oleanane-type triterpenic acid was isolated from the leaves of Gymnema sylvestre(Asclepiadaceae). The structure was characterized as 3β, 16β, 22β, 28-tetrahydroxy- olean-12-en-30-oic acid on the basis of spectral evidence, including 1D- and 2D-NMR (HMQC, HMBC, H-1H 1COSY and NOESY).展开更多
P-glycoprotein(P-gp)is an important transmembrane ATP-binding cassette(ABC)drug efflux transporter expressed in various human tissues such as the intestines,liver,kidneys,and bloodbrain barrier.It limits the intracell...P-glycoprotein(P-gp)is an important transmembrane ATP-binding cassette(ABC)drug efflux transporter expressed in various human tissues such as the intestines,liver,kidneys,and bloodbrain barrier.It limits the intracellular concentration of xenobiotics by pumping them out of the cells,affecting drug pharmacokinetics and therapeutic effects.With its broad substrate specificity,it has the potential to remove a wide range of drugs from Chinese materia medica(CMM),including conventional medicines and active compounds.Increasing evidence has confirmed the superior therapeutic effectiveness of CMM in treating a wide range of diseases worldwide,as well as in conjunction with western drugs.As a result,herbal medicine-drug compounds have prompted widespread concern,with the majority of these interactions involving transporters such as P-gp.This review systematically summarizes the inhibition or induction of P-gp expression/function by active CMM compounds and the underlying regulatory mechanisms.It will aid in improving understanding of the synergistic or inhibiting effects associated with transporter P-gp as well as rational safety concerns for using CMM,particularly in combination with drugs.展开更多
Chuanwu(CW), a famous traditional Chinese medicine(TCM) from the mother roots of Aconitum carmichaelii Debx..(Ranunculaceae), has been used for the treatment of various diseases. Unfortunately, its toxicity is frequen...Chuanwu(CW), a famous traditional Chinese medicine(TCM) from the mother roots of Aconitum carmichaelii Debx..(Ranunculaceae), has been used for the treatment of various diseases. Unfortunately, its toxicity is frequently reported because of its narrow therapeutic window. In the present study, a metabolomic method was performed to characterize the phenotypically biochemical perturbations and potential mechanisms of CW-induced toxicity. Meanwhile, the expression level of toxicity biomarkers in the urine were analyzed to evaluate the detoxification by combination with Gancao(Radix Glyeyrrhizae, CG), Baishao(Radix Paeoniae Alba, CS) and Ganjiang(Rhizoma Zingiberis, CJ), which were screened from classical TCM prescriptions. Urinary metabolomics was performed by UPLC-Q-TOF-HDMS, and the mass spectra signals of the detected metabolites were systematically analyzed using pattern recognition methods. As a result, seventeen biomarkers associated with CW toxicity were identified, which were associated with pentose and glucuronate interconversions, alanine, aspartate, and glutamate metabolism, among others. The expression levels of most toxicity biomarkers were effectively modulated towards the normal range by the compatibility drugs. It indicated that the three compatibility drugs could effectively detoxify CW. In summary, our work demonstrated that metabolomics was vitally significant to evaluation of toxicity and finding detoxification methods for TCM.展开更多
This study was aimed at evaluating the anti-diabetic potential of passion fruit Passiflora edulis(EPE) extracts in diabetic rats, following Streptozotocin(STZ) induced oxidative stress. Thirty adult Wistar rats were d...This study was aimed at evaluating the anti-diabetic potential of passion fruit Passiflora edulis(EPE) extracts in diabetic rats, following Streptozotocin(STZ) induced oxidative stress. Thirty adult Wistar rats were divided into five groups, with six rats in each group. The control rats were injected intraperitoneally with citrate buffer(pH 4.5). The remaining groups of rats were administered single dose of 45 mg·kg-1 of STZ by intraperitoneal route to induce diabetes. The diabetic animals were treated with 250 and 500 mg·kg-1 of EPE and glibenclamide 0.6 mg·kg-1 for fifteen days by oral route. Blood glucose, end organ oxidative stress marker, and anti-oxidants were assayed. Further, histopathological investigation of pancreas was studied at the end of the experimentation. The results revealed that subacute administration of EPE significantly(P < 0.001) controlled the blood glucose level in the diabetic rats. In addition, EPE extract protected the end organs by restoring the anti-oxidants enzyme, significantly increasing super oxide dismutase level(SOD) and decreasing catalase(CAT) and TBARS level in visceral organs. In conclusion, that EPE extracts showed anti-diabetic and anti-oxidant potential against streptozotocin-induced diabetes.展开更多
The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L.(Thymelaeaceae) that is used in traditional Chinese medicine(TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isoch...The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L.(Thymelaeaceae) that is used in traditional Chinese medicine(TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand(–)-gossypol through 3D similarity search. It selectively bound to Bcl-xL and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L-1 and 9.98 ± 0.21 μmol·L-1, respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L-1 and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L-1. Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L..展开更多
Platycodin D(PD), a triterpenoid saponin isolated from Platycodonis Radix, is a famous Chinese herbal medicine that has been shown to have anti-proliferative effects in several cancer cell lines. The aim of this study...Platycodin D(PD), a triterpenoid saponin isolated from Platycodonis Radix, is a famous Chinese herbal medicine that has been shown to have anti-proliferative effects in several cancer cell lines. The aim of this study was to determine the changes in cellular proteins after the treatment of hepatocellular carcinoma HepG2 cells with PD using proteomics approaches. The cell viability was determined using the MTT assay. The proteome was analyzed by two-dimensional difference gel electrophoresis and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. Western blot analysis was used to confirm the expression of changed proteins. Our results showed that PD inhibited the proliferation of HepG2 cells in concentration- and time-dependent manners. Sixteen proteins were identified to be up-regulated in PD-treated HepG2 cells, including ATP5 H, OXCT1, KRT9, CCDC40, ERP29, RCN1, ZNF175, HNRNPH1, HSP27, PA2G4, PHB, BANF1, TPM3, ECH1, LGALS1, and MYL6. Three proteins(i.e., RPS12, EMG1, and KRT1) decreased in HepG2 cells after treatment with PD. The changes in HSP27 and PHB were further confirmed by Western blotting. In conclusion, our results shed new lights on the mechanisms of action for the anti-cancer activity of PD.展开更多
Many phytochemicals show promise in cancer prevention and treatment, but their low aqueous solubility, poor stability, unfavorable bioavailability, and low target specificity make administering them at therapeutic dos...Many phytochemicals show promise in cancer prevention and treatment, but their low aqueous solubility, poor stability, unfavorable bioavailability, and low target specificity make administering them at therapeutic doses unrealistic. This is particularly true for(-)-epigallocatechin gallate, curcumin, quercetin, resveratrol, and genistein. There is an increasing interest in developing novel delivery strategies for these natural products. Liposomes, micelles, nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers and poly(lactide-co-glycolide) nanoparticles are biocompatible and biodegradable nanoparticles. Those nanoparticles can increase the stability and solubility of phytochemicals, exhibit a sustained release property, enhance their absorption and bioavailability, protect them from premature enzymatic degradation or metabolism, prolong their circulation time, improve their target specificity to cancer cells or tumors via passive or targeted delivery, lower toxicity or side-effects to normal cells or tissues through preventing them from prematurely interacting with the biological environment, and enhance anti-cancer activities. Nanotechnology opens a door for developing phytochemical-loaded nanoparticles for prevention and treatment of cancer.展开更多
Two new naphthalenone compounds were isolated from green walnut husks of Juglans mandshurica and their structures were identified as 4-butoxybutoxy-5,8-dihydroxy-3,4-dihydro-2H-naphthalen-1-one(1), 4-ethoxyethoxy-5,8-...Two new naphthalenone compounds were isolated from green walnut husks of Juglans mandshurica and their structures were identified as 4-butoxybutoxy-5,8-dihydroxy-3,4-dihydro-2H-naphthalen-1-one(1), 4-ethoxyethoxy-5,8-dihydroxy-3,4-dihydro-2H-naphthalen-1-one(2). Compounds 1 and 2 were named as Juglanstetralone A(1) and Juglanstetralone B(2). Compound 1 showed more significant anti-tumor activity than 2 against gastric cancer BGC-823 cells, wih the IC50 of 125.89 ?g?mL –1.展开更多
Maca(Lepidium meyenii) is an herbaceous plant that grows in high plateaus and has been used as both food and folk medicine for centuries because of its benefits to human health. In the present study, ITS(internal tran...Maca(Lepidium meyenii) is an herbaceous plant that grows in high plateaus and has been used as both food and folk medicine for centuries because of its benefits to human health. In the present study, ITS(internal transcribed spacer) sequences of forty-three maca samples, collected from different regions or vendors, were amplified and analyzed. The ITS sequences of nineteen potential adulterants of maca were also collected and analyzed. The results indicated that the ITS sequence of maca was consistent in all samples and unique when compared with its adulterants. Therefore, this DNA-barcoding approach based on the ITS sequence can be used for the molecular identification of maca and its adulterants.展开更多
The present study was designed to investigate the role of quercetin on neurite growth in N1E-115 cells and the underlying mechanisms. Quercetin was evaluated for its effects on cell numbers of neurites, neurite length...The present study was designed to investigate the role of quercetin on neurite growth in N1E-115 cells and the underlying mechanisms. Quercetin was evaluated for its effects on cell numbers of neurites, neurite length, intracellular cAMP content, and Gap-43 expression in N1E-115 cells in vitro by use of microscopy, LANCE? cAMP 384 kit, and Western blot analysis, respectively. Our results showed that quercetin could increase the neurite length in a concentration-dependent manner, but had no effect on the numbers of cells. Quercetin significantly increased the expression of cellular cAMP in a time- and concentration-dependent manner. The Gap-43 expression was up-regulated in a time-dependent manner. In conclusion, quercetin could promote neurite growth through increasing the intracellular c AMP level and Gap-43 expression.展开更多
Xingxiong injection(XXI) is a widely used Chinese herbal formula prepared by the folium ginkgo extract and ligustrazine for the treatment of cardiovascular and cerebrovascular diseases. Compared with the pharmacologic...Xingxiong injection(XXI) is a widely used Chinese herbal formula prepared by the folium ginkgo extract and ligustrazine for the treatment of cardiovascular and cerebrovascular diseases. Compared with the pharmacological studies, chemical analysis and quality control studies on this formula are relatively limited. In the present study, a high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry(HPLC-QTOF MS) method was applied to comprehensive analysis of constituents in XXI. According to the fragmentation rules and previous reports, thirty ginkgo flavonoids, four ginkgo terpene lactones, and one alkaloid were identified. A high performance liquid chromatography coupled with triple quadrupole mass spectrometry(HPLC-QQQ MS) method was then applied to quantify ten major constituents in XXI. The method validation results indicated that the developed method had desirable specificity, linearity, precision and accuracy. The total contents of ginkgo flavonoids were about 22.05-25.51 μg·mL-1 and the ginkgo terpene lactones amounts were about 4.41-8.70 μg·m L-1 in six batches of XXI samples, respectively. Furthermore, cosine ratio algorithm and distance measurements were employed to evaluate the similarity of XXI samples, and the results demonstrated a high-quality consistency. This work could provide comprehensive information on the quality control of Xingxiong injection, which be helpful in the establishment of a rational quality control standard.展开更多
The present study was designed to isolate and evaluate the antibacterial activity of the compounds from the whole plant of Euphorbia helioscopia L.. Various chromatographic techniques were used to isolate and purify t...The present study was designed to isolate and evaluate the antibacterial activity of the compounds from the whole plant of Euphorbia helioscopia L.. Various chromatographic techniques were used to isolate and purify the compound. The structure of the compound was elucidated on basis of spectral data(1H NMR, 13 C NMR, 1H-1H COSY, HSQC, HMBC, NOESY, IR, and HR-ESI-MS). A new jatrophone-type diterpenoid(14α,15β-diacetoxy-3β-benzoyloxy-7β-nicotinoyloxy-9-oxo-jatropha-5E,11E-diene), named euphoheliosnoid E(1), was isolated from the whole plant of E. helioscopia L. Compound 1 showed significant anti-microbial activity against oral pathogens.展开更多
文摘Deep visceral pain is frequent and presents major challenges in pain management, since its pathophysiology is still poorly understood. One way to optimize treatment of visceral pain is to improve knowledge of the mechanisms behind the pain and the mode of action of analgesic substances. This can be achieved through stand-ardized experimental human pain models. Experimental pain models in healthy volunteers are advantageous for evaluation of analgesic action, as this is often diff icult to assess in the clinic because of confounding factors such as sedation, nausea and general malaise. These pain models facilitate minimizing the gap between knowledge gained in animal and human clinical studies. Combining experimental pain studies and pharmacokinetic stud- ies can improve understanding of the pharmacokinetic-pharmacodynamic relationship of analgesics and, thus, provide valuable insight into optimal clinical treatment of visceral pain. To improve treatment of visceral pain, it is important to study the underlying mechanisms of pain and the action of analgesics used for its treatment. An experimental pain model activates different modalities and can be used to investigate the mechanism of action of different analgesics in detail. In combination with pharmacokinetic studies and objective assessment such as electroencephalography, new information re-garding a given drug substance and its effects can be obtained. Results from experimental human visceral pain research can bridge the gap in knowledge between animal studies and clinical condition in patients suffering from visceral pain, and thus constitute the missing link in translational pain research.
基金Supported by the Postdoctoral Science Foundation of China, No. [2001] 5
文摘AIM: To investigate the antitumor and synergistic effect of Chinese medicine “Bushen huayu jiedu recipe” (recipe for invigorating the kidney, removing blood stasis and toxic substances) and chemotherapy on mice hepatocarcinoma. METHODS: Bushen huayu jiedu recipe (BSHYJDR) consisting of Chinese Cassia Bark, Psoralea, Zedoary, Rhubarb, etc. is equal to 1.5 g/mL liquid of originated herbs after being decoded, filtered, and concentrated. Kunming mice, weighing 18-22 g, were injected with 0.2 mL ascitic hepatocarcinoma H22 containing 1 × 10^7 cells/mL into armpit of the right forelimb of mice. After 24 h, the mice were weighed and randomly divided into tumor-bearing model control group, cisplatin (DDP) group, BSHYJDR high dosage group, low dosage BSHYJDR group, DDP combined with high and low dosage BSHYJDR group, 10 mice in each group. DDP group received injection intraperitoneally (ip) at the dosage of 1 mg/kg (equal to 1/10 LD50), once a day for 4 d. High and low dosage BSHYJDR groups received intragastric BSHYJDR at the dosages of 26.6 and 13.3 g/kg (20 and 10 times each of clinical adult dosage) respectively, while tumor-bearing model group received the equal volume of distilled water once a day for 10 d. On the 11^th d, the mice were weighed and killed, then the tumor was dissected and weighed, the repression rate (RR) was calculated according to the mean weight of tumor (MWT). RESULTS: Compared to the model group (MWT: 1.30±0.73), DDP group (MWT: 0.41±0.09, RR: 68.46%) had a significant difference in the inhibition of hepatocarcinoma H22 (P〈0.01). High dosage BSHYJDR group (MWT: 0.69±0.29, RR: 46.92%) also had a significant difference in inhibition (P〈0.05), while no difference was found in low dosage BSHYJDR group (MVVT: 0.85±0.34, RR: 34.62%) (P〉0.05). When DDP was combined with high dosage BSHYJDR (MWT: 0.29±0.17, RR: 77.69%) and low dosage BSHYJDR (MWT: 0.38±0.21, RR: 70.77%) respectively, we could see improvement of the inhibition effect of DDP on transplanted hepatocarcinoma H22. DDP combined with high dosage BSHYJDR had a significant difference (P〈0.001) compared to DDP, while DDP combined with low dosage BSHYJDR only had a little improvement that is not remarkable. CONCLUSION: Chinese medicine BSHYJDR in combination with chemotherapy can inhibit transplanted hepatocarcinorna in mice.
文摘A novel oleanane-type triterpenic acid was isolated from the leaves of Gymnema sylvestre(Asclepiadaceae). The structure was characterized as 3β, 16β, 22β, 28-tetrahydroxy- olean-12-en-30-oic acid on the basis of spectral evidence, including 1D- and 2D-NMR (HMQC, HMBC, H-1H 1COSY and NOESY).
基金the Macao Science and Technology Development Fund(No.0067/2019/A2 and No.0075/2019/AMJ)from the Macao Special Administrative Region。
文摘P-glycoprotein(P-gp)is an important transmembrane ATP-binding cassette(ABC)drug efflux transporter expressed in various human tissues such as the intestines,liver,kidneys,and bloodbrain barrier.It limits the intracellular concentration of xenobiotics by pumping them out of the cells,affecting drug pharmacokinetics and therapeutic effects.With its broad substrate specificity,it has the potential to remove a wide range of drugs from Chinese materia medica(CMM),including conventional medicines and active compounds.Increasing evidence has confirmed the superior therapeutic effectiveness of CMM in treating a wide range of diseases worldwide,as well as in conjunction with western drugs.As a result,herbal medicine-drug compounds have prompted widespread concern,with the majority of these interactions involving transporters such as P-gp.This review systematically summarizes the inhibition or induction of P-gp expression/function by active CMM compounds and the underlying regulatory mechanisms.It will aid in improving understanding of the synergistic or inhibiting effects associated with transporter P-gp as well as rational safety concerns for using CMM,particularly in combination with drugs.
基金supported by the Key Program of National Natural Science Foundation of China(Nos.81430093,81173500,81373930,81302905,81102556,and 81202639)National Key Subject of Drug Innovation(Nos.2015ZX09101043-005 and 2015ZX09101043-011)+1 种基金Heilongjiang University of Chinese Medicine Scientific Research Fund Projects(No.201307)Application Technology and Development of Youth Talents Project of Harbin,China(2014RFQXJ116)
文摘Chuanwu(CW), a famous traditional Chinese medicine(TCM) from the mother roots of Aconitum carmichaelii Debx..(Ranunculaceae), has been used for the treatment of various diseases. Unfortunately, its toxicity is frequently reported because of its narrow therapeutic window. In the present study, a metabolomic method was performed to characterize the phenotypically biochemical perturbations and potential mechanisms of CW-induced toxicity. Meanwhile, the expression level of toxicity biomarkers in the urine were analyzed to evaluate the detoxification by combination with Gancao(Radix Glyeyrrhizae, CG), Baishao(Radix Paeoniae Alba, CS) and Ganjiang(Rhizoma Zingiberis, CJ), which were screened from classical TCM prescriptions. Urinary metabolomics was performed by UPLC-Q-TOF-HDMS, and the mass spectra signals of the detected metabolites were systematically analyzed using pattern recognition methods. As a result, seventeen biomarkers associated with CW toxicity were identified, which were associated with pentose and glucuronate interconversions, alanine, aspartate, and glutamate metabolism, among others. The expression levels of most toxicity biomarkers were effectively modulated towards the normal range by the compatibility drugs. It indicated that the three compatibility drugs could effectively detoxify CW. In summary, our work demonstrated that metabolomics was vitally significant to evaluation of toxicity and finding detoxification methods for TCM.
文摘This study was aimed at evaluating the anti-diabetic potential of passion fruit Passiflora edulis(EPE) extracts in diabetic rats, following Streptozotocin(STZ) induced oxidative stress. Thirty adult Wistar rats were divided into five groups, with six rats in each group. The control rats were injected intraperitoneally with citrate buffer(pH 4.5). The remaining groups of rats were administered single dose of 45 mg·kg-1 of STZ by intraperitoneal route to induce diabetes. The diabetic animals were treated with 250 and 500 mg·kg-1 of EPE and glibenclamide 0.6 mg·kg-1 for fifteen days by oral route. Blood glucose, end organ oxidative stress marker, and anti-oxidants were assayed. Further, histopathological investigation of pancreas was studied at the end of the experimentation. The results revealed that subacute administration of EPE significantly(P < 0.001) controlled the blood glucose level in the diabetic rats. In addition, EPE extract protected the end organs by restoring the anti-oxidants enzyme, significantly increasing super oxide dismutase level(SOD) and decreasing catalase(CAT) and TBARS level in visceral organs. In conclusion, that EPE extracts showed anti-diabetic and anti-oxidant potential against streptozotocin-induced diabetes.
基金supported by the National Natural Science Foundation of China(Nos.81302651,81230090,and 81222046)the Fundamental Research Funds for the Central Universities(No.222201314041)+3 种基金the Global Research Network for Medicinal Plants(GRNMP)King Saud University,the Shanghai Leading Academic Discipline Project(No.B906)the Key Laboratory of Drug Research for Special Environments,PLA,the Shanghai Engineering Research Center for the Preparation of Bioactive Natural Products(No.10DZ2251300)the Scientific Foundation of Shanghai China(Nos.12401900801,09DZ1975700,09DZ1971500,and 10DZ1971700)
文摘The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L.(Thymelaeaceae) that is used in traditional Chinese medicine(TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand(–)-gossypol through 3D similarity search. It selectively bound to Bcl-xL and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L-1 and 9.98 ± 0.21 μmol·L-1, respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L-1 and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L-1. Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L..
基金supported by the Science and Technology Development Fund,Macao S.A.R(FDCT)(070/2013/A)the Research Fund of University of Macao(SRG026-ICMS13-LJJ and MRG008-LJJ2014-ICMS)+1 种基金the Administration of Traditional Chinese Medicine of Zhejiang Province(No.2012 ZA028)Program of Xinmiao Talents in Zhejiang Province(No.2010 R410024)
文摘Platycodin D(PD), a triterpenoid saponin isolated from Platycodonis Radix, is a famous Chinese herbal medicine that has been shown to have anti-proliferative effects in several cancer cell lines. The aim of this study was to determine the changes in cellular proteins after the treatment of hepatocellular carcinoma HepG2 cells with PD using proteomics approaches. The cell viability was determined using the MTT assay. The proteome was analyzed by two-dimensional difference gel electrophoresis and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. Western blot analysis was used to confirm the expression of changed proteins. Our results showed that PD inhibited the proliferation of HepG2 cells in concentration- and time-dependent manners. Sixteen proteins were identified to be up-regulated in PD-treated HepG2 cells, including ATP5 H, OXCT1, KRT9, CCDC40, ERP29, RCN1, ZNF175, HNRNPH1, HSP27, PA2G4, PHB, BANF1, TPM3, ECH1, LGALS1, and MYL6. Three proteins(i.e., RPS12, EMG1, and KRT1) decreased in HepG2 cells after treatment with PD. The changes in HSP27 and PHB were further confirmed by Western blotting. In conclusion, our results shed new lights on the mechanisms of action for the anti-cancer activity of PD.
基金supported by grant from the National Center for Complementary&Integrative Health(Nos.R15AT007013 and R15AT008733)
文摘Many phytochemicals show promise in cancer prevention and treatment, but their low aqueous solubility, poor stability, unfavorable bioavailability, and low target specificity make administering them at therapeutic doses unrealistic. This is particularly true for(-)-epigallocatechin gallate, curcumin, quercetin, resveratrol, and genistein. There is an increasing interest in developing novel delivery strategies for these natural products. Liposomes, micelles, nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers and poly(lactide-co-glycolide) nanoparticles are biocompatible and biodegradable nanoparticles. Those nanoparticles can increase the stability and solubility of phytochemicals, exhibit a sustained release property, enhance their absorption and bioavailability, protect them from premature enzymatic degradation or metabolism, prolong their circulation time, improve their target specificity to cancer cells or tumors via passive or targeted delivery, lower toxicity or side-effects to normal cells or tissues through preventing them from prematurely interacting with the biological environment, and enhance anti-cancer activities. Nanotechnology opens a door for developing phytochemical-loaded nanoparticles for prevention and treatment of cancer.
基金supported by Major National Drug Program(No.2010ZX09102-138)the Innovation Fund for Youth Science and Technology in Harbin(No.2012RFQYS042)
文摘Two new naphthalenone compounds were isolated from green walnut husks of Juglans mandshurica and their structures were identified as 4-butoxybutoxy-5,8-dihydroxy-3,4-dihydro-2H-naphthalen-1-one(1), 4-ethoxyethoxy-5,8-dihydroxy-3,4-dihydro-2H-naphthalen-1-one(2). Compounds 1 and 2 were named as Juglanstetralone A(1) and Juglanstetralone B(2). Compound 1 showed more significant anti-tumor activity than 2 against gastric cancer BGC-823 cells, wih the IC50 of 125.89 ?g?mL –1.
基金supported by the High-Tech Research Program–863 Program in China(No.2012AA021702-4)
文摘Maca(Lepidium meyenii) is an herbaceous plant that grows in high plateaus and has been used as both food and folk medicine for centuries because of its benefits to human health. In the present study, ITS(internal transcribed spacer) sequences of forty-three maca samples, collected from different regions or vendors, were amplified and analyzed. The ITS sequences of nineteen potential adulterants of maca were also collected and analyzed. The results indicated that the ITS sequence of maca was consistent in all samples and unique when compared with its adulterants. Therefore, this DNA-barcoding approach based on the ITS sequence can be used for the molecular identification of maca and its adulterants.
基金supported by the National Natural Science Foundation of China(No.81271338)Specialized Research Fund for Doctoral Program of Higher Education of China(No.20130096 110011)
文摘The present study was designed to investigate the role of quercetin on neurite growth in N1E-115 cells and the underlying mechanisms. Quercetin was evaluated for its effects on cell numbers of neurites, neurite length, intracellular cAMP content, and Gap-43 expression in N1E-115 cells in vitro by use of microscopy, LANCE? cAMP 384 kit, and Western blot analysis, respectively. Our results showed that quercetin could increase the neurite length in a concentration-dependent manner, but had no effect on the numbers of cells. Quercetin significantly increased the expression of cellular cAMP in a time- and concentration-dependent manner. The Gap-43 expression was up-regulated in a time-dependent manner. In conclusion, quercetin could promote neurite growth through increasing the intracellular c AMP level and Gap-43 expression.
基金supported by the National Natural Science Foundation of China(Nos.81473343 and 81202898)Project in the National Science&Technology Pillar Program during the Twelfth Five-year Plan Period(No.2012BAI29B07)+2 种基金Program for New Century Excellent Talents in University(No.NECT-13-1034)Natural Science Foundation of Jiangsu Province(No.BK20130652)a Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘Xingxiong injection(XXI) is a widely used Chinese herbal formula prepared by the folium ginkgo extract and ligustrazine for the treatment of cardiovascular and cerebrovascular diseases. Compared with the pharmacological studies, chemical analysis and quality control studies on this formula are relatively limited. In the present study, a high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry(HPLC-QTOF MS) method was applied to comprehensive analysis of constituents in XXI. According to the fragmentation rules and previous reports, thirty ginkgo flavonoids, four ginkgo terpene lactones, and one alkaloid were identified. A high performance liquid chromatography coupled with triple quadrupole mass spectrometry(HPLC-QQQ MS) method was then applied to quantify ten major constituents in XXI. The method validation results indicated that the developed method had desirable specificity, linearity, precision and accuracy. The total contents of ginkgo flavonoids were about 22.05-25.51 μg·mL-1 and the ginkgo terpene lactones amounts were about 4.41-8.70 μg·m L-1 in six batches of XXI samples, respectively. Furthermore, cosine ratio algorithm and distance measurements were employed to evaluate the similarity of XXI samples, and the results demonstrated a high-quality consistency. This work could provide comprehensive information on the quality control of Xingxiong injection, which be helpful in the establishment of a rational quality control standard.
基金supported by the Fundamental Research Funds for the Central Universities(No.JB-ZR1226)the National Natural Science Foundation of China(No.81202940)
文摘The present study was designed to isolate and evaluate the antibacterial activity of the compounds from the whole plant of Euphorbia helioscopia L.. Various chromatographic techniques were used to isolate and purify the compound. The structure of the compound was elucidated on basis of spectral data(1H NMR, 13 C NMR, 1H-1H COSY, HSQC, HMBC, NOESY, IR, and HR-ESI-MS). A new jatrophone-type diterpenoid(14α,15β-diacetoxy-3β-benzoyloxy-7β-nicotinoyloxy-9-oxo-jatropha-5E,11E-diene), named euphoheliosnoid E(1), was isolated from the whole plant of E. helioscopia L. Compound 1 showed significant anti-microbial activity against oral pathogens.